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Assay Detail

CHEMBL980652

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Functional
Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS binding
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of arylalkoxy- and biarylalkoxy-phenylamide and phenylimidazoles as potent and selective sphingosine-1-phosphate receptor subtype-1 agonists.
Evindar G, Satz AL, Bernier SG, Kavarana MJ, Doyle E, Lorusso J, Taghizadeh N, Halley K, Hutchings A, Kelley MS, Wright AD, Saha AK, Hannig G, Morgan BA, Westlin WF.
Bioorg Med Chem Lett (2009) 19 : 2315 -2319
PubMed 19282175 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.02 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL514302 1 9.28
CHEMBL473238 1 8.96
CHEMBL474418 1 8.66
CHEMBL475253 1 8.57
CHEMBL473156 1 8.54
CHEMBL515917 1 8.14
CHEMBL470511 1 7.99
CHEMBL473562 1 7.43
CHEMBL514170 1 7.43
CHEMBL473563 1 7.36
CHEMBL475405 1 7.25
CHEMBL515603 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL514302 EC50 = 0.52 nM 9.28
CHEMBL473238 EC50 = 1.1 nM 8.96
CHEMBL474418 EC50 = 2.2 nM 8.66
CHEMBL475253 EC50 = 2.67 nM 8.57
CHEMBL473156 EC50 = 2.9 nM 8.54
CHEMBL515917 EC50 = 7.3 nM 8.14
CHEMBL470511 EC50 = 10.2 nM 7.99
CHEMBL473562 EC50 = 37.0 nM 7.43
CHEMBL514170 EC50 = 37.2 nM 7.43
CHEMBL473563 EC50 = 44.1 nM 7.36
CHEMBL475405 EC50 = 56.1 nM 7.25
CHEMBL515603 EC50 = 247.0 nM 6.61